4000-520-616
欢迎来到免疫在线！(蚂蚁淘生物旗下平台)  请登录 |  免费注册 |  询价篮
产品库 品牌馆 现货促销 技术交流 新闻动态 联系我们
MedChemExp
主营：主营：抑制剂、激动剂、API
咨询热线电话
4000-520-616
公司首页 公司介绍 产品中心 新闻动态 联系方式 在线下单
当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/H-89二盐酸盐（同义词：蛋白激酶抑制剂H-89二盐酸盐）/HY-15979A/50mg
商品详细Medchemexpress/H-89二盐酸盐（同义词：蛋白激酶抑制剂H-89二盐酸盐）/HY-15979A/50mg
Medchemexpress/H-89二盐酸盐（同义词：蛋白激酶抑制剂H-89二盐酸盐）/HY-15979A/50mg
Medchemexpress/H-89二盐酸盐（同义词：蛋白激酶抑制剂H-89二盐酸盐）/HY-15979A/50mg
商品编号： HY-15979A-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1480.00
美元价： 888.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
立即询价
商品介绍
H-89(dihydrochloride)isapotentinhibitorofcyclicAMP-dependentproteinkinase(proteinkinaseA)withIC50of48nMandhasweakinhibitiononPKG,PKC,CaseinKinase,andotherskinases.
Description

H-89(dihydrochloride)isapotentinhibitorofcyclicAMP-dependentproteinkinase(proteinkinaseA)withIC50of48nMandhasweakinhibitiononPKG,PKC,CaseinKinase,andotherskinases.

IC50&Target

IC50:48nM(proteinkinaseA)

InVitro

H-89inhibitsproteinkinaseA,incompetitivefashionagainstATP.H-89causesadose-dependentinhibitionoftheforskolin-inducedproteinphosphorylation,withnodecreaseinintracellularcyclicAMPlevelsinPC12Dcells.H-89significantlyinhibitstheforskolin-inducedneuriteoutgrowthfromPC12Dcells.H-89(30μM)inhibitssignificantlycAMP-dependenthistoneIIbphosphorylationactivityinPC12Dcelllysates[1].H-89(1-2μM)significantlyslowsthereprimingrateinratskinnedfibres,mostlikelyduetoitdeleteriouslyaffectingtheT-systempotential.H-89(10-100μM)inhibitsnetCa2+uptakebytheSRandaffectestheCa2+-sensitivityofthecontractileapparatusinratskinnedfibres[2].

InVivo

H-89(0.2mg/100g,i.p.)significantlyincreasesseizurelatencyandthresholdinPTZ-treatedanimals.H-89(0.05,0.2mg/100g,i.p.)preventstheepileptogenicactivityofbucladesine(300nM)withsignificantincreaseofseizurelatencyandseizurethreshold[3].

References

  • [1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D

    [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.

    [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9257mL9.6287mL19.2574mL
5mM0.3851mL1.9257mL3.8515mL
10mM0.1926mL0.9629mL1.9257mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

Kinaseactivitiesareassayedat30°Cfor2-5minbymeasuringthetransferof32Pfrom[γ-32P]ATPtosubstrates.Thereactionisterminatedbyadding1mLof20%trichloroaceticacid,followingtheadditionof100μgofbovineserumalbuminasacarrierprotein.Thesampleiscentrifugedat3000rpmfor10min,thepelletisresUSPendedin5%trichloroaceticacidsolution,thefinalpelletisdissolvedin1mLof1NNaOHandtherADIoactivityismeasuredinaliquidscintillationcounter.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

After48hinculture,PCl2Dcellsareculturedintestmediumcontaining30μMH-89for1handthenexposedtofreshmediumthatcontainedboth10μMforskolinand30μMH-89.Cellsarescrapedoffwitharubberpolicemanandsonicatedinthepresenceof0.5mLof6%trichloroaceticacid.Toextracttrichloroaceticacid,2mLofpetroleumetherisadded,thepreparationmixedandcentrifugedat3000rpmfor10min.Afteraspirationoftheupperlayer,theresiduesamplesolutionisusedfordetermination.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

H-89isdissolvedinDMSOanddistilledwater(10%).

Malealbinomiceweighing20-25gareobtained.Pentoxifylline(25,50,100mg/kg),bucladesine(50,100,300nM/mouse)andH-89(0.05,0.1,0.2mg/100g)areadministeredintraperitoneally(i.p.)30minbeforeintravenous(i.v.)infusionofPTZ.Incombinationgroups,thefirstandsecondcomponentsareinjected45and30minbeforePTZinfusion.Inallgroups,therespectivecontrolanimalsreceiveanappropriatevolumeofvehicle.Forthei.v.infusion,theneedleisinsertedintothelateraltailvein,fixedtothetailveinbyanarrowpieceofadhesivetape,andtheanimalisallowedtomovefreely.PTZsolutionisinfusedataconcentrationrateof1mL/min.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D

    [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.

    [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

MolecularWeight

519.28

Formula

C₂₀H₂₂BrCl₂N₃O₂S

CASNo.

130964-39-5

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥50mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.94%